Coix seeds are dried ripe seeds of Coix lacryma-jobi L. var ma-yuen (Roman.), Stapf, a genus of plant in the Poaceae family. It is a dampness-eliminating drug and has been used as a medicinal and edible plant for a long time. Modern researches have found that Coix seeds have many pharmacological effects, such as analgesic, anti-inflammatory, immunomodulatory, anti-ulcer, hypolipidemic and anti-obesity effects. In recent years, researchers around the world have studied the chemical composition of the Coix seed by using TLC, HPLC-MS, GC, etc., and found a variety of active ingredients in it, including coixenolide, triglycerides, fatty acids, lactams, coix lactones, saccharides, sterols and triterpenoids. Among them, esters are the first discovered components having anti-tumor activities and the most reported chemical composition attracting the most attention. Kanglaite injection, in which the active ingredient is Coix seed oil, has been widely used in present Chinese clinical applications. However, there is rarely report on the substance basis and active antitumor ingredients. Xiang zhiming, at al, have analyzed qualitatively triglycerides in Coix seed oil and presumed tentatively 12 triglycerides: trilinolein, olein-dilinolein, palmitin-dilinolein, diolein-linolein, palmitin-linolein-olein, dipalmitin-linolein, triolein, olein-linolein-stearin, palmitin-diolein, palmitin-linolein-stearin, dipalmitin-olein and diolein-stearin (China Journal of Chinese Materia Medica, 2005, 30 (18): 1436-1438). However, they have not further studied the specific chemical structures and pharmacological activities of these ingredients. In fact, Coix seed oil also contains monoglycerides, diglycerides and fatty acid esters, etc. It can be seen that Coix seed contains complex components. This will inevitably be a great challenge for the quality control in the practical production process and the safety in clinical applications.
Therefore, the development of a safe, effective and controllable medicine for the treatment of tumors and the immuno-enhancement became a focused issue of the invention. In the present invention, diglyceride and triglyceride ingredients have been isolated from Coix seed oil one by one, their structures have been confirmed and their pharmaceutical activities have been screened. Among them, the inventors have selected 13 glycerides having obvious antitumor and immuno-enhancement. These 13 glycerides have been combined in different ratios and their pharmacodynamic tests have been conducted. Thus, the pharmaceutical composition of the invention and pharmaceutical preparations thereof have been obtained, and the uses thereof in the treatment of tumors and in the immuno-enhancement have been provided. The use of the pharmaceutical composition of the invention, having confirmed ingredients and definite composition, in medication can ensure the stability of quality in each batch in the industrial production and avoid toxic and side effects induced by the complication of ingredients in crude Coix seed oil when it is directly adopted.